Flutamide for hirsutism
Flutamide is a potent antiandrogen that strongly binds to androgen receptors on cells in hair follicles and anywhere else in the body. Even though it binds to the cell receptors it does not stimulate the cells into any response. When naturally produced androgens bind to the same receptors on hair follicle cells, the cells may respond with increased activity and terminal hair production. The binding of Flutamide to cell androgen receptors blocks the receptors from binding to naturally produced androgens and so stops natural androgens from stimulating hair growth.
Studies that compare flutamide to spironolactone or cyproterone acetate suggest that overall the beneficial effects on reducing hirsutism are similar. Some suggest flutamide is slightly superior and others say it is slightly less superior. Initially flutamide was given to patients at high dose rates of up to 250mg three times a day. However more recent studies indicate that a similar improvement in hirsutism can be obtained with flutamide doses as low as 62.5mg a day. The reduction in dose significantly reduces the risk of side effects.
For a small subgroup of women flutamide and other oral antiandrogens are highly toxic. Between February 1989 and December 1994 the Food and Drug Administration (FDA) received reports of 20 patients who died and 26 who were hospitalized for hepatotoxicity due to flutamide, a rate around 3 per 10,000 flutamide users. Early symptoms of hepatotoxicity include nausea, vomiting, fatigue and jaundice and if such symptoms occur they must be immediately reported to a doctor. Dermatologists generally recommend that serial blood aminotransferase levels should be monitored during the first few months of flutamide treatment. Any adverse aminotransferase level changes suggest that hepatotoxicity is a significant risk and flutamide use should be stopped. For this and other reasons, some dermatologists do not use flutamide to treat hirsutism however, the side effect risk of flutamide is no better or worse than other oral antiandrogens
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